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Estradiol‐antagonistic activity of phenolic compounds from leguminous plants
Author(s) -
Pinto B.,
Bertoli A.,
Noccioli C.,
Garritano S.,
Reali D.,
Pistelli L.
Publication year - 2008
Publication title -
phytotherapy research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.019
H-Index - 129
eISSN - 1099-1573
pISSN - 0951-418X
DOI - 10.1002/ptr.2327
Subject(s) - genistein , luteolin , flavones , daidzein , isoflavones , chemistry , phytoestrogens , antagonist , yeast , flavonoid , stereochemistry , biochemistry , biology , estrogen , receptor , endocrinology , chromatography , antioxidant
Natural flavonoids are currently receiving much attention because of their estrogenic and antiestrogenic properties. Six isoflavones (isoprunetin, isoprunetin 7‐ O ‐ β ‐ d ‐glucopyranoside, isoprunetin 4′,7‐di‐ O ‐ β ‐ d ‐glucopyranoside, genistein, genistein 7‐O‐ β ‐ d ‐glucopyranoside, daidzein), four flavones (luteolin, luteolin 7‐O‐ β ‐ d ‐glucopyranoside, luteolin 4′‐O‐ β ‐ d ‐glucopyranoside, licoflavone C), isolated from Genista morisii and G. ephedroides (two Leguminosae plants of the Mediterranean area) together with two structurally related pterocarpans, bitucarpin A and erybraedyn C, isolated from Bituminaria bituminosa (Leguminosae), were tested for the antagonist activity by a yeast based estrogen receptor assay ( Saccharomyces cerevisiae RMY326 ER‐ERE). Most compounds inhibited the estradiol‐induced transcriptional activity in a concentration dependent manner. In particular, for the flavone luteolin 77% inhibition of the induced β ‐galactosidase activity was observed. Interestingly, licoflavone C exhibited a dose‐dependent antagonistic activity at concentrations up to 10−4 m , but stimulated β ‐galactosidase expression at higher concentrations resulting in a U‐shaped‐like dose‐response curve. Copyright © 2007 John Wiley & Sons, Ltd.